Compounds for the treatment of SARS
Inhibitors of SARS-COV-2 (COVID), pharmaceutical compositions comprising same; and methods of treating a severe acute respiratory syndrome.
1 . A compound of the formula (I):
or a pharmaceutically acceptable salt thereof, wherein:
R 1 —O-1 to 4 carbon alkylene-6 to 10 membered aryl 6 to 10-membered heterocyclyl with one heteroatom or —O-1 to 4 carbon alkylene-6 to 10-membered heterocyclyl with one heteroatom, wherein the 6 to 10-membered heterocyclyl with one heteroatom is connected via a carbon atom on the 6 to 10-membered heterocyclyl group;
R 2 is alkyl, aryl, substituted aryl;
R 3 is 5-or 6-membered heterocyclyl with one to four heteroatoms, wherein the 5- or 6-membered heterocyclyl with one to four heteroatoms is connected to the —CH 2 - group via a carbon atom on the 5- or 6-membered heterocyclyl group with one to four heteroatoms;
R 4 is H, alkyl or alkenyl; and
R a is H or alkyl,
or a pharmaceutically acceptable salt thereof.
2 . The compound of claim 1 , wherein the compound is a compound of the formula (IIa) or (IIb):
or a pharmaceutically acceptable salt thereof,
wherein:
m is 1 or 2; and
R 4 is methyl or —CH 2 —C(H)CH 2 .
3 . The compound of claim 1 , wherein R 1 is:
4 . The compound of claim 1 , wherein R 4 is methyl or —CH 2 —C(H)CH 2 .
5 . The compound of claim 1 , wherein R 4 is H.
6 . The compound of claim 1 , wherein the compound of formula (I) is a compound of the formula:
or a pharmaceutically acceptable salt thereof.
7 . The compound of claim 1 , wherein the compound of formula (I) is a compound of the formula:
or a pharmaceutically acceptable salt thereof.
8 . The compound of claim 1 , wherein the compound of formula (I) is a compound of the formulae:
or a pharmaceutically acceptable salt thereof.
9 . The compound of claim 1 , wherein the compound of formula (I) is a compound of the formula:
or a pharmaceutically acceptable salt thereof.
10 . The compound of claim 1 , wherein the compound of formula (I) is a compound of the formulae;
or a pharmaceutically acceptable salt thereof.
11 . A pharmaceutical composition comprising a therapeutically effective amount of one or more compounds of claim 1 and at least one pharmaceutically acceptable excipient.
12 . A method for treating a severe acute respiratory syndrome, the method comprising administering a therapeutically effective amount of one or more compounds of claim 1 or a pharmaceutical composition comprising one or more compounds of claim 1 to a patient in need thereof, whereupon the patient is treated for a severe acute respiratory syndrome.
13 . The method of claim 12 , wherein the severe acute respiratory syndrome is COVID-19.